MEDCHEM FINAL QUIZ DRUGS

Anti-fibrinolytic agent

INT: treatment of clyclic heavy menstrual bleeding

Ovulation and Gonadotropin Stimulants

• Treatment of ovarian failure and male infertility
• Increase pituitary output of gonadotropins

• INT: prepubertal cryptorchidism, hypogonadism,
• ovulation stimulation

INT: final follicular maturation, ovulation induction

Polypeptide with chorionic gonadotropin activity

INT: primary hypothalamic amenorrhea

Polypeptide with chorionic gonadotropin activity

• INT: precocious puberty (early puberty) and
• endometriosis

Polypeptide with chorionic gonadotropin activity

INT: central precocious puberty

• Recombinant form of human luteinizing hormone from
• hampsters

• INT: Stimulation of follicular development in
• hypogonadotropic hypogonal women with luteinizing hormone deficiency

• INT: treatment of advanced prostate cancer to
• achieve medical castration

• MOA: direct and competitive inhibitor of
• gonadotropin releasing hormone receptors in pituitary

Only doctors with PLUS program may prescribe

Small quantities in females

Primary sex hormones of males 2 types of activity

• Androgenic activity – male sex characteristic
• promotion

Anabolic activity – muscle building activity

• Two natural hormones – testosterone and
• 5alpha-dihydrotestosterone

Androgen replacement therapy in men

• Testosterone deficiency through hypogonadism or
• hypopituitarism

Low doses in women to treat postpartum breast enlargement

• Selected use in women for advanced or metastatic carcinoma
• of the breast

• Used to treat certain anemias, osteoporosis, and
• stimulate growth in post-puberty boys

• Anabolics contraindicated in men with family
• history of prostate or testicular cancer

• DI: incrase anticoagulant activity, interference
• with lab tests

Short acting testosterone product

INT: Hypogonadism

Long acting testosterone products

Prodrugs

Flouxymestrone

Danazol

• INT: endometriosis, fibrocystic breast disease,
• hereditary angioedema

MOA: inhibits pituitary gonadotropins

• INT: begign prostatic hyperplasia, androgenic
• alopecia

• MOA: Inhibits conversion of testosterone to
• 5alpha-dihydrotestosterone via 5alpha-reductase inhibition

INT: benign prostatic hyperplasia

• MOA: Inhibits conversion of testosterone to
• 5alpha-dihydrotestosterone via 5alpha-reductase inhibition

Nonsteroidal

INT: Benign prostatic hyperplasia

• MOA: selective blockade of smooth muscle
• post-synaptic alpha1-adronergic receptors

50% reduction in absorption w/o food

Extensively metabolized by CYP3A4

Nonsteroidal

INT: benign prostatic hyperplasia

• MOA: selective blockade/antagonism of smooth
• muscle post-synaptic alpha1a-adrenergic receptors

Take with food

Steroids used for anabolic activity

• INT: adjuctive to promote weight gain after
• surgery, chronic infections, severe trauma, HIV wasting syndrome

Steroids used for anabolic activity

INT: Anemias

Steroids used for anabolic activity

INT: anemias of renal insufficiency

INT: hereditary angioedema

Human plasma kallkrein inhibitor

SubQ

INT: acute attacks of hereditary angioedema

MOA: Directly inhibiting kallikrein

Watch for anaphylaxis

INT: acute attacks of hereditary angioedema

MOA: selective bradykinin B2 receptor antagonist

Nonsteroidal used for anemia

• INT: transfusion-dependent anemia due to low or
• intermediate risk myelodysplastic syndrome (MDS)

Teratogenic

• Adverse effects: neutropenia, thrombocytopenia,
• increased risk of blood clots and pulmonary emboli

Uterine-active agents

Abortifacients

• BLACK BOX: may cause life threatening infection
• due to incomplete abortion

MOA: Progesterone antagonist

New indication for Cushing’s Disease

• MOA: antagonist of one of the body’s two cortisol
• receptors and progesterone receptors

• Useful in treating psychosis and depression
• associated with Cushing’s

Abortifacient

• MOA: stimulates uterine contractions, used in
• conjuction with surgical methods such as saline-injections or suction abortion

INT: labor induction in conjuction with oxytocin

MOA: stimulates uterine contractions

INT: induction of labor via IV drip

• MOA: natural pituitary hormone that increases
• uterine contractions

Post-partum or postabortal bleeding

• MOA: partial antagonist/agonist of
• alpha-adrenergic, dopaminergic or tryptaminergic receptor of uterine tissue
• increasing uterine contractions and decreasing bleeding

Post-partum or post-abortal bleeding

INT: management of pre-term labor

• MOA: a beta2-receptor agonist that decreases
• uterine smooth muscle contractions

• Slow the formation and dissolution of
• hydroxyapatite crystals

• MOA: bisphosphonate is incorporated into the bone
• matrix and is imbibed by osteoclasts. This incapacitates the osteoclast
• preventing resorption of the bone

• INT: paget’s disease, malignancy induced
• hypercalcemia, postmenopausal osteoporosis, metastatic cancer of the bone,
• ossification caused by injury or total hip replacement

• Use caution in renal impairment, avoid Al and Mg
• containing antacids, may cause nausea and diarrhea

Etidronate

Pamidronate

Alendronate

Tiludronate sodium

Risendronate Sodium

New Biphosphonate product

• INT: hypercalcemia due to malignancy, IV once
• yearly for osteoporosis and paget’s
• disease

New bisphosphonate product

Indicated postmenopausal osteoporosis

• INT: treatment of osteoporosis in both men and
• women at increased risk of fracture

• MOA: a recombinant human parathyroid hormone,
• unique in that it actually stimulates new bone formation

Increased risk of osteosarcoma

SubQ injection

• INT: treatment of postmenopausal women with
• osteoporosis at high risk of fracture

MOA: RANK ligand inhibitor

Injection given once every six months

New calcimimetic

• INT: treatment of secondary hyperparathyroidism
• dialysis patients with chronic kidney disease, hypercalcemia secondary to
• parathyroid carcinoma

• MOA: increases the sensitivity of the Ca+2
• sensing receptor on parathyroid gland chief cells that regulate the production
• of PTH

Major mineralcorticoid is aldosterone

Major glucocorticoid is cortisol

Release regulated by ACTH secretions by the pituitary

• Primary adrenocortical insufficiency – requires replacement
• therapy of both glucocorticoids and mineralcorticoids

• Secondary adrenocortical insufficiency – Due to
• inadequate ACTH secretion

• Caused by excessive secretion of glucocorticoids as
• a result of excessive ACTH secretions or a primary adrenal source such as a
• tumor

• Best treatment is surgical but adrenal steroid
• inhibitors can be used

Caused by prolonged treatment with glucocorticoids

• Common symptoms: euphoria, buffalo hump, thinning
• of the skin, increased abdominal fat, Thin arms and legs with muscle wasting,
• increased bruising and poor wound healing, moon face w/ read cheeks

Increased susceptibility to infection

• Adrenal steroid inhibitor (prevents the conversion
• of cholesterol to pregnenolone)

• INT: Cushing’s syndrome, postmenopausal patients
• with advanced breast and prostate carcinoma

ACTH injection and a repository product

• INT: diagnostic testing of adrenal function ,
• nonsupprurative thyroiditis, hypercalcemia associated with cancer, acute
• multiple sclerosis

Glucocorticoid product

Mineralcorticoid product

• INT: primary or secondary adrenal insufficiency,
• management of severe orthostatic hypotension

INT: rheumatoid arthritis

MOA: inhibitor of de novo pyrimidine synthesis

• Contraindications: pregnancy or desire to get
• pregnant

Prodrug

Can be used to treat growth failure

Recombinant insulin-like growth factor 1

• INT: treatment of growth failure in children with
• severe primary insulin-like growth factor

INT: acromegaly, tumors, GI fistula, diarrheal states, hypoglycemia due to excess insulin

INT: long-term treatment of acromegalic patients who have had an inadequate response to or cannot be treated with surgery or radiotherapy

Orphan Drug

Treatment of hereditary tyrosinemia type 1

• Caution: results in elevated plasma levels of
• tyrosine so must watch diet

Isolated from salmon

• INT: used in postmenopausal osteoporosis, paget’s
• disease, hypercalcemia

• MOA: Calcitonin suppresses resorption of bone by
• inhibiting the ctivity of osteoclasts

Must be coadministered with Calcium

INT: euvolemic hyponatremia – too little Na present in the blood stream but normal amount of fluid

MOA: non-peptide, dual antagonist of arginine vasopressin receptors

INT: hypervolemic and euvolemic hyponatremia patients with HF, cirrhosis and inappropriate antidiuretic hormone secretion

MOA: oral selective vasopressin-receptor antagonist

Metabolized by CYP3A